Structure–activity relationships of trimethoxybenzyl piperazine N-type calcium channel inhibitors

…, L Zhang, H Pajouhesh, X Jiang, A Hendricson…

文献索引：Pajouhesh, Hassan; Feng, Zhong-Ping; Zhang, Lingyun; Pajouhesh, Hossein; Jiang, Xinpo; Hendricson, Adam; Dong, Haiheng; Tringham, Elizabeth; Ding, Yanbing; Vanderah, Todd W.; Porreca, Frank; Belardetti, Francesco; Zamponi, Gerald W.; Mitscher, Lester A.; Snutch, Terrance P. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 12 p. 4153 - 4158

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被引用次数: 18

摘要

We previously reported the small organic N-type calcium channel blocker NP078585 that while efficacious in animal models for pain, exhibited modest L-type calcium channel selectivity and substantial off-target inhibition against the hERG potassium channel. Structure–activity studies to optimize NP078585 preclinical properties resulted in compound 16, which maintained high potency for N-type calcium channel blockade, and possessed ...